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Phamacology Summer > Pharmacologic Principles Part 1: Pharmaceutics, Pharmacokinetics > Flashcards

Pharmacologic Principles Part 1: Pharmaceutics, Pharmacokinetics Flashcards

1
Q

Study of drugs (pharmacokinetics and pharmacodynamics)

Pharmakon or Pharmacology

A

Pharmacology

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2
Q

Comes from Greek word “Pharmakon”

Pharmakon or Pharmacology

A

Pharmacology

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3
Q

Means drug(remedy) and poison

Pharmakon or Pharmacology

A

Pharmakon

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4
Q

Drug affects the body

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACEUTICS

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5
Q

Body does to the drug

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACOKINETICS

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6
Q

Drug does to the body

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACODYNAMICS

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7
Q

“Peanut Butter”

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACOKINETICS

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8
Q

“Jelly”

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACODYNAMICS

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9
Q

Drug absorption fast to slowest.

a. Enteric Coated Tablets
b. Capsules
c. Oral disintegration, Buccal Tablets, & Oral Soluble Wafers
d. Powder
e. Tablets
f. Liquids, elixers, & syrups
g. Coated Tablets
h. Suspension Solution

A

c. Oral disintegration, Buccal Tablets, & Oral Soluble Wafers
f. Liquids, elixers, & syrups
h. Suspension Solution
d. Powder
b. Capsules
e. Tablets
g. Coated Tablets
a. Enteric Coated Tablets

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10
Q

Already in dissolved form and thus absorbed quickly

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Oral Liquids/Suspensions

b. Oral Liquids/Suspensions

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11
Q

Extra coating on the outside prevents drug from being broken down by the acidic pH of the
stomach

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Enteric Coated Tablets

a. Enteric Coated Tablets

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12
Q

Drug is not absorbed until they reach the small intestine (higher pH)

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Enteric Coated Tablets

a. Enteric Coated Tablets

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13
Q

Commonly made to PROTECT the gastric mucosa from irritation

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Enteric Coated Tablets

a. Enteric Coated Tablets

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14
Q

Release drug over a prolonged period of time

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Extended Release/Sustained Release Tablets

e. Extended Release/Sustained Release Tablets

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15
Q

◦ Abbreviations => EC

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Enteric Coated Tablets

a. Enteric Coated Tablets

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16
Q

◦ Abbreviations => SR, SA, CR, XL, XT, ER, and more

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Extended Release/Sustained Release Tablets

e. Extended Release/Sustained Release Tablets

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17
Q

Sublingual, Buccal

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Oral Mucosa Absorption

d. Oral Mucosa Absorption

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18
Q

Absorbed through surface of the skin
◦ Skin, Eyes, Ears, Nose, Rectum, Vagina, Lungs and more

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Topical/Transdermal

f. Topical/Transdermal

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19
Q

IV formulations must have similar pH to blood, otherwise damage can happen to veins/arteries

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Parenteral (Injectable)

c. Parenteral (Injectable)

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20
Q

◦ Drug is immediately in solution (no need to dissolve)

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Parenteral (Injectable)

c. Parenteral (Injectable)

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21
Q

◦ Therefore drug is 100% absorbed and ready to work!

a. Enteric Coated Tablets
b. Oral Liquids/Suspensions
c. Parenteral (Injectable)
d. Oral Mucosa Absorption
e. Extended Release/Sustained Release Tablets
f. Topical/Transdermal

A

Parenteral (Injectable)

c. Parenteral (Injectable)

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22
Q 
PHARMACOKINETICS
body does to the drug (ADME)
A-
D-
M-
E-
A

Absorption
Distribution
Metabolism
Elimination/Excretion

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23
Q

ADME

PHARMACOKINETICS, PHARMACEUTICS, or PHARMACODYNAMICS

A

PHARMACOKINETICS

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24
Q

Study of what happens to a parent drug from the time it is put into the body until the parent drug and all metabolites have left the body

Nursing process, ADME, QSEN, or IPEC

A

ADME

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25
Q

Movement of a drug from its site of administration into the bloodstream for distribution to the tissues

Elimination/Excretion
Distribution
Absorption
Metabolism

A

Absorption

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26
Q

Bioavailability
First Pass Effect
P-Glycoprotein
Routes

Elimination/Excretion
Distribution
Absorption
Metabolism

A

Absorption

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27
Q

Percentage of how much active drug reaches the bloodstream

P-Glycoprotein
Bioavailability
Routes
First Pass Effect

A

Bioavailability

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28
Q 
Which is true 
Oral Route is 100% Bioavailable
IV Route is 100% Bioavailable
Oral Route is variable
IV Route is variable
A

IV Route is 100% Bioavailable

Oral Route is variable

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29
Q

What influences bioavailability?

a. P-Glycoproteins
b. First Pass Effect
c. Oral Route/GI Tract factor
d. And more!
e. None
f. All

A

f. All

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30
Q

First Pass Effect in order

a. Metabolized drug reaches general blood circulation
b. Drugs can get absorbed in GI tract
▪ gastric mucosa (stomach)
▪ Intestinal mucosa (small intestines)
c. The gastric/intestinal mucosal blood flow goes to portal vein
d. Swallow the drug orally
e. Portal Vein carries the blood to the Liver
f. Liver metabolizes drugs (FIRST PASS EFFECT)
g. Drug travels down the GI tract

A

d. Swallow the drug orally
g. Drug travels down the GI tract
b. Drugs can get absorbed in GI tract
▪ gastric mucosa (stomach)
▪ Intestinal mucosa (small intestines)
c. The gastric/intestinal mucosal blood flow goes to portal vein
e. Portal Vein carries the blood to the Liver
f. Liver metabolizes drugs (FIRST PASS EFFECT)
a. Metabolized drug reaches general blood circulation

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31
Q 
Mouth-
Stomach-
Small Intestines-
Large Intestines-
Rectum-

Liver or GBC (General Blood Circulation)

A 
Mouth- GBC
Stomach- Liver
Small Intestines- Liver
Large Intestines- Liver
Rectum- GBC
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32
Q

Part of our “defense system”

a. P-Glycoproteins
b. First Pass Effect
c. Oral Route/GI Tract factor
d. And more!
e. None
f. All

A

a. P-Glycoproteins

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33
Q

Located in essentials areas of body
◦ Blood Brain Barrier, GI Tract

a. P-Glycoproteins
b. First Pass Effect
c. Oral Route/GI Tract factor
d. And more!
e. None
f. All

A

a. P-Glycoproteins

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34
Q

Called - “Anti-absorption pumps” or Efflux Pumps

a. P-Glycoproteins
b. First Pass Effect
c. Oral Route/GI Tract factor
d. And more!
e. None
f. All

A

a. P-Glycoproteins

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35
Q

▪P-glycoproteins (More or Less)

a. Net Result= More absorption of drugs into the general circulation
b. Net Result= Less absorption of drugs into the general circulation

A

Less

b. Net Result= Less absorption of drugs into the general circulation

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36
Q

P-Glycoprotein

Inhibitor or Inducer?

A

Inhibitor

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37
Q

P-Glycoprotein Inhibitor:

Cranberry Juice
Grape Fruit

A

Grape Fruit

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38
Q

The drug is absorbed into the systemic circulation through the GI tract

Enteral or Parental

A

Enteral

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39
Q

Oral
Sublingual/Buccal
Suppositories

Enteral or Parental

A

Enteral

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40
Q

The most common of all routes is the ORAL ROUTE
▪ Most drugs are ABSORBED in stomach or small intestine

Enteral or Parental

A

Enteral

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41
Q

What can influence ORAL route ABSORPTION?

a. pH of the GI tract
b. Drugs or Meals
c. Drug Formulation
d. None

A

a. pH of the GI tract
b. Drugs or Meals
c. Drug Formulation

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42
Q

◦ Drug is placed under the tongue

Buccal or Sublingual

A

Sublingual

43
Q

◦ Drug is placed between the cheek and gum

Buccal or Sublingual

44
Q

◦ EXAMPLE: NitroSTAT- Nitroglycerin tablets used for acute chest pain (heart attack or angina)

Buccal or Sublingual

A

Sublingual

45
Q

◦ EXAMPLE: Actiq®- Essentially a fentanyl lollipop for acute, extreme breakthrough cancer pain

Buccal or Sublingual

46
Q

Key Points: For Buccal & Sublingual

a. Drug is absorbed in the oral mucosa of the mouth and goes directly into the blood stream
b. Must allow the drug to dissolve
c. Swallowing the medication may inactivate the medication (pH of stomach)
d. Do not eat or drink until medication has dissolved
e. None
f. All

47
Q

(Non GI-Tract administration, aka Injections)

Enteral or Parental

48
Q

◦ The drug is absorbed into the systemic circulation via injections

Enteral or Parental

49
Q

Intravenous (FASTEST!)
Intramuscular/Subcutaneous/Intradermal
Epidural- Spinal cord injection

Enteral or Parental

50
Q

Epidural

Enteral or Parental

51
Q

Inhalation
Topical/Transdermal
Instillation (eye/ear/nose drops/sprays)

Enteral or Parental

52
Q 
•KEY CONCEPTS
1. Permeability of the Cell Membrane
◦ Lipid Soluble vs Water Soluble
◦ Blood Brain Barrier, Placenta
2. Protein Binding of drugs
◦ Free vs Bound Drug
3. Circulation/Blood Supply
◦ Diseases that alter circulation

Which ADME

A

DISTRIBUTION

53
Q

▪PERMEABILITY OF CELL MEMBRANE
◦ Easily distribute into fatty tissues where they may store or concentrate

Water or Lipid Soluble

A

Lipid Soluble

54
Q

▪PERMEABILITY OF CELL MEMBRANE
◦ Have the potential to cross the Blood Brain Barrier (BBB) and the Placenta

Water or Lipid Soluble

A

Lipid Soluble

55
Q

▪PERMEABILITY OF CELL MEMBRANE
◦ Typically remain in highly vascularized spaces and can easily leave the body via elimination (urine!)

Water or Lipid Soluble

56
Q

▪PROTEIN BINDING
◦ Albumin is the most common blood protein
◦ Some drugs preferentially bind to protein/albumin
◦ Called

Highly or Lowly bound drugs“

57
Q

Drug is not bound to albumin
◦ can distribute into extravascular tissue to its intended target

Bound drug or Free drug

58
Q

Stuck to albumin, stays in the bloodstream
◦ Cannot get to extravascular space and reach intended target

Bound drug or Free drug

A

Bound drug

59
Q

◦ Free drug

Active or Inactive

60
Q

◦ Bound drug

Active or Inactive

61
Q

What are potential complications of Highly Protein Bound Drugs?

a. Deficiency in Protein/Albumin
b. Competition (two drugs can result in toxicity)
c. None
d. All

62
Q

▪CIRCULATION/BLOOD SUPPLY
Vital organs like the heart, kidneys, liver, brain

Slow or Rapid

63
Q

▪CIRCULATION/BLOOD SUPPLY
Muscle, skin, fat

Slow or Rapid

64
Q

▪CIRCULATION/BLOOD SUPPLY
CONCERNS/ALTERATIONS

a. Diseases/Conditions can alter perfusion
b. Peripheral Vascular Disease, Heart Diseases (Heart Failure
c. None
d. All

65
Q 
Metabolism/Biotransformation
Cytochrome P-450
Enzyme Induction
Enzyme Inhibition
Pro-Drug
First Pass Effect

Which ADME

A

Metabolism

66
Q

BIOTRANSFORMATION = which ADME

A

Metabolism

67
Q

The biochemical alteration of a drug (substrate= target drug)

Which ADME

A

Metabolism

68
Q

(substrate= ?)

A

target drug

69
Q

Which of the following are true about metabolism?

a. convert drug into an active metabolite or inactive metabolite
b. Metabolites could be weaker or stronger than the original drug
c. Liver is primary organ
d. Minor roles: Skeletal muscle, Kidneys, Lungs, Plasma, Intestinal mucosa
e. None
f. All

70
Q

IMPORTANT REMINDER : NOT ALL DRUGS GO THROUGH METABOLISM

True or False

71
Q

Convert drugs to become hydrophilic and polar.

P-Glycoproteins or Cytochrome P-450 (CYP450)

A

Cytochrome P-450 (CYP450)

72
Q

Liver enzymes target drugs (substrates)

P-Glycoproteins or Cytochrome P-450 (CYP450)

A

Cytochrome P-450 (CYP450)

73
Q

◦ Typically target drugs that are lipophilic and non polar

P-Glycoproteins or Cytochrome P-450 (CYP450)

A

Cytochrome P-450 (CYP450)

74
Q

Both Enzyme Induction, Enzyme Inhibition

P-Glycoproteins or Cytochrome P-450 (CYP450)

A

Cytochrome P-450 (CYP450)

75
Q

Which are METABOLISM ALTERATION

a. Other drugs
b. Certain Foods (Grape Fruit)
c. Smoking/Alcohol
d. Patient variables
e. Diseases (liver diseases)
f. Genetics*
g. Age
h. None
i. All

76
Q

METABOLISM ALTERATION

Age
◦ Infants have (limited or unlimited) liver enzymes
◦ Geriatric patients may have (less or more) liver enzyme activity

A

Age
◦ Infants have limited liver enzymes
◦ Geriatric patients may have less liver enzyme activity

77
Q

Inducers:

PS – PORCS or PACMAN loves Grapefruit juice!

A

PS – PORCS

78
Q

Inhibitors:

PS – PORCS or PACMAN loves Grapefruit juice!

A

PACMAN loves Grapefruit juice!

79
Q

Inducers: PS – PORCS

P- phenytoin
N- non-DHP Calcium Channel Blockers (diltiazem, verapamil)
A- amiodarone
R- rifampin
C- carbamazepine
S- St. John’s Wort (OTC herb)
P- phenobarbita
O- Oxcarbazepine
A- azole antifungal (fluconazole, ketoconazole)
C- cimetidine (H2RAs)
P- protease inhibitor (HIV)
M- macrolides (ACE, Azithromycin, Clarithromycin, Erythromycin)
S- Smoking
G- Grape Juice
A 
P – phenytoin
S – Smoking
P – phenobarbital
O – Oxcarbazepine
R – rifampin
C –carbamazepine
S – St. John’s Wort (OTC herb)
80
Q

Inhibitors: PACMAN loves Grapefruit juice!

P- phenytoin
N- non-DHP Calcium Channel Blockers (diltiazem, verapamil)
A- amiodarone
R- rifampin
C- carbamazepine
S- St. John’s Wort (OTC herb)
P- phenobarbita
O- Oxcarbazepine
A- azole antifungal (fluconazole, ketoconazole)
C- cimetidine (H2RAs)
P- protease inhibitor (HIV)
M- macrolides (ACE, Azithromycin, Clarithromycin, Erythromycin)
S- Smoking
G- Grape Juice
A

P – protease inhibitor (HIV)
A – azole antifungal (fluconazole, ketoconazole)
C – cimetidine (H2RAs)
M – macrolides(ACE, Azithromycin, Clarithromycin, Erythromycin)
A – amiodarone
N – non-DHP Calcium Channel Blockers (diltiazem, verapamil)
♥’s
Grapefruit juice

81
Q

HEPATOCYTES

Kidney or Liver

82
Q

◦ Metabolism of drugs (CYP enzymes)

Kidney or Liver

83
Q

◦ Metabolism of hormones

Kidney or Liver

84
Q

◦ Protein Synthesis and degradation

Kidney or Liver

85
Q

◦ Coagulation- uses Vitamin K to make clotting factors

Kidney or Liver

86
Q

◦ Albumin

Kidney or Liver

87
Q

◦ Glycogen storage (Glycogenesis)

Kidney or Liver

88
Q

◦ Cholesterol- Lipids + Bile Acid metabolism

Kidney or Liver

89
Q

▪ Cirrhosis

Kidney or Liver

90
Q

▪ Hepatotoxicity

Kidney or Liver

91
Q

▪ DRUGS (Drug Induced Liver Injury- DILI), Alcoholic Liver Disease, Hepatitis, more!

Kidney or Liver

92
Q

◦ Dark urine- (bilirubin mixes with urine)

Kidney or Liver

93
Q

Jaundice (yellow eyes, liver no longer filters bilirubin from blood, or can’t conjugate it so it can’t be removed via bile)

Kidney or Liver

94
Q

Swelling of abdomen (no longer making sufficient albumin)

Kidney or Liver

95
Q

Bruising/Bleeding (lack of clotting factors)
◦ Fatigue

Kidney or Liver

96
Q

Ammonia can concentrate (liver normally converts to urea)

Kidney or Liver

97
Q

◦ Ammonia accumulation- neurological changes- encephalopathy

Kidney or Liver

98
Q

PHARMACOKINETICS: METABOLISM

Kidney or Liver

99
Q

PHARMACOKINETICS: ELIMINATION

Kidney or Liver

100
Q

Other Mechanisms:
◦ Liver, Breast milk, Sweat, Bowel (biliary excretion, enterohepatic recirculation)

METABOLISM or ELIMINATION

A

ELIMINATION

101
Q

Injury to the kidney which results in a
sudden elevated SCr/BUN and a decreased eGFR/CrCl

Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

A

Acute Kidney Injury

102
Q

Chronically elevated SCr/BUN,
decreased eGFR/CrCl

Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

A

Chronic Kidney Disease

103
Q

Certain drugs may be harmful to the kidneys.
We call the resulting damage, nephrotoxicity. Clinically, this is also called an acute kidney injury

Chronic Kidney Disease, Acute Kidney Injury, or Nephrotoxicity

A

Nephrotoxicity

Phamacology Summer (48 decks)

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